Drug Transporter Pharmacogenomics – When it Matters and When it Doesn’t?

Session Description

Drug transporters on cell membranes play critical roles in regulating substrate exposure in systemic circulation and peripheral tissues. Therefore, genetic polymorphisms in drug transporters could impact pharmacokinetic and pharmacodynamic variability. Understanding how, when, and what considerations of the drug transporter polymorphisms can impact response during drug development are important for clinical pharmacologists. This session will focus on the recent growing body of research elucidating the role of genetic polymorphisms in major drug transporters of the intestine and liver, namely BCRP, OATP1B1 and OCT1. The overall goal of the session is to educate clinical pharmacologists about the mechanisms by which coding and non-coding variants in these transporters affect transporter function and impact drug absorption and elimination. The participants will acquire new knowledge of recent approved drugs that are impacted by polymorphisms of these transporters and how it affects prescribing information labelling. Participants will learn about the resources, such as the FDA Table of Pharmacogenetic Associations, as well as how and when prescribing information needs to include transporter polymorphisms. Finally, participants will learn how clinical research is conducted in humans to improve understanding the impact of drug transporter genetic polymorphisms on drug pharmacokinetics and pharmacodynamics variability. The session include Q&A and polling questions to engage attendees.

Learning Objectives

1. Describe the mechanisms by which genetic polymorphisms in drug transporters alter drug absorption and elimination.

2. Give at least two examples in which transporter polymorphisms should be considered in patients and highlighted in drug prescribing information documents.

Session Schedule

11:00 AM - 11:02 AM ET
Introduction
Kit Wun Kathy Cheung, PharmD and Shuiying Hu, PhD

11:02 AM - 11:16 AM ET
Exploring the Impact of OATP1B1 Functional Polymorphisms in Non-European Populations
Sook Wah Yee, PhD

11:16 AM - 11:30 AM ET
Translating Impact of OCT1 on Drug Variability – From Genetics to Biomarkers
Mladen V. Tzvetkov, PhD

11:30 AM - 11:44 AM ET
Regulatory Considerations for Pharmacogenetic Interactions in Labeling
Katarzyna Drozda, PharmD

11:44 AM - 12:00 PM ET
Q&A and Closing Remarks